Abstract
A novel subclass of quinolones, 2-pyridones, showed potent activity against Mycobacterium tuberculosis, with KRQ-10018 being an early lead. KRQ-10018 showed better activity in vitro against M. tuberculosis versus moxifloxacin. In vivo efficacy of KRQ-10018 at 300 mg/kg of body weight was similar to that of isoniazid at 25 mg/kg, but showed less activity than moxifloxacin at 300 mg/kg.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Antitubercular Agents / administration & dosage
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Antitubercular Agents / pharmacology*
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Antitubercular Agents / therapeutic use*
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Biological Availability
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Interferon-gamma / genetics
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Mice
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Mice, Inbred C57BL
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Mice, Knockout
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Microbial Sensitivity Tests
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Mycobacterium tuberculosis / drug effects*
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Pyridones / administration & dosage
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Pyridones / pharmacology*
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Pyridones / therapeutic use*
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Quinolones / administration & dosage
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Quinolones / pharmacology
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Quinolones / therapeutic use
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Treatment Outcome
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Tuberculosis, Pulmonary / drug therapy*
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Tuberculosis, Pulmonary / microbiology
Substances
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Antitubercular Agents
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Pyridones
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Quinolones
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2-hydroxypyridine
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Interferon-gamma